102 results about "Fluorouracilum" patented technology

The invention discloses an enantiokaurane compound with antitumor activity as well as a preparation method and application of the enantiokaurane compound. According to the present invention, chemical components of Western African plant I.trichantha tubers are deeply studied, and a variety of chromatographic separation methods such as macroporous resin, silica gel resin, medium pressure preparation-MCI column, gel normal pressure column and semi-preparative high performance liquid chromatography are combined to separate to obtain one enantiokaurane new compound Trichanthone B; experiments show that the compound obtained through separation has a good inhibition effect on an MIA PaCa-2 pancreatic cancer cell line and an A549 lung cancer cell line, and IC50 of the compound on the MIA PaCa-2 pancreatic cancer cell line reaches a nanomole level; the effect of the compound is stronger than that of positive drugs 5-fluorouracil and carboplatin, and the compound has the potential of being developed into new drugs for resisting pancreatic cancer and lung cancer.

The invention discloses synthesis and antitumor activity research of a novel drug small molecular formula (1) containing a phenothiazine structure. R is # imgabs 1 #. 10H phenothiazine is used as an initial raw material, (E)-3-(10-ethyl-10H-phenothiazin-3-yl) acrylic acid is generated through a typical Friedel-Crafts alkylation reaction, an NBS bromination reaction and the like, and then an important intermediate compound 6 is synthesized through a Wittig reaction and a hydrolysis reaction. And carrying out coupling reaction on the intermediate compound 7 and different amine compounds to obtain 11 target compounds 7a-7k: formula (1). A CCK-8 experiment is carried out on a target compound to obtain a conclusion that the target compound 7a-7k and 5-fluorouracil are tested at the concentration of 20 mu M, and the result shows that the compound 7f has the best inhibition effect on A549, Hep G2 and HeLa cells, and the compound 7c has the better inhibition effect on the A549 cells. IC50 value calculation is carried out on a target compound under various concentrations, the IC50 value of 7c to HELA cells is small, the IC50 value of 7f to Hep G2 and HeLa cells is minimum, and the inhibition effect is the best. Therefore, the compound can be used for antitumor drugs.

The invention discloses an application of homocapsaicin II in preparation of an anti-tumor drug, the homocapsaicin II is used in the anti-tumor drug independently or in combination with 5-fluorouracil or in combination with oxaliplatin, and when the homocapsaicin II is used in preparation of an anti-colorectal cancer drug, the drug concentration is 20-200 [mu] M. It is found that high capsaicin II can inhibit growth of intestinal cancer cells in vivo and in vitro, and nude mice have good tolerance to the natural compound. When the compound is used together with a first-line chemotherapeutic drug 5-fluorouracil, the drug concentration of the 5-fluorouracil can be remarkably reduced while the same treatment effect is achieved, a synergistic cancer inhibition effect is achieved, and a new research and development approach is found for anti-colorectal cancer drugs.

The invention provides a gastric cancer prognosis marker and application thereof, and belongs to the technical field of biology. According to the invention, survival analysis is carried out to explore the prognosis correlation of m6A'write 'RBM15 in gastric cancer. The result proves that the RBM15 is a prognostic marker related to a better clinical result and can be used for judging the prognosis condition of a gastric cancer patient. The invention verifies the relationship among RBM15, ECT2 and EMT signal pathway, and the result proves that RBM15 mediates m6A methylation of ECT2 through IGF2BP3, affects the stability of ECT2 RNA, affects the expression of ECT2, and regulates EMT signal pathway at the same time. The invention further discloses a mechanism of the RBM15 for influencing proliferation, invasion and migration of gastric cancer cells and sensitivity to 5-fluorouracil chemotherapy, and a new therapeutic target is provided for gastric cancer treatment.

This invention relates to a pharmaceutical composition for tumor treatment and its application. Specifically, this invention relates to a composition containing a fluorouracil drug and pyrimidine nucleosides and their derivatives. Fluorouracil drugs and pyrimidine nucleotides and their derivatives have a synergistic antitumor effect; combined use can reduce the concentration of single drugs and achieve better antitumor efficacy, while reducing toxic side effects.

The application provides a combination drug of a PLA2G7 inhibitor and a chemotherapeutic drug and its use in resisting triple-negative breast cancer, and belongs to the technical field of medicines. The combination drug is a PLA2G7 inhibitor and a chemotherapeutic drug in the same or different specifications of unit preparations for simultaneous or separate administration, and a pharmaceutically acceptable carrier. The application first discovers and proves that the PLA2G7 inhibitor Darapladib can significantly enhance the anti-tumor activity of paclitaxel, 5-fluorouracil or cisplatin on triple-negative breast cancer, and meanwhile, the combination of the PLA2G7 inhibitor and paclitaxel has a synergistic effect in down-regulating the phosphorylation level of STAT3 protein in cancer cells and inhibiting the growth and proliferation of cancer cells; the combination of the PLA2G7 inhibitor and 5-fluorouracil also shows a synergistic effect in inhibiting the growth and proliferation of cancer cells. The application provides a new and effective combination drug strategy for improving the treatment effect of the chemotherapeutic drug on triple-negative breast cancer.

The application relates to a synthesis method of red luminescent carbon dots with a targeting diagnosis and treatment potential of hepatocellular carcinoma, which comprises the following steps: 1) adding 5-fluorouracil and indocyanine green into deionized water, uniformly mixing, and forming a uniform mixed solution; 2) heating the mixed solution obtained in the step 1) at 160-200 DEG C for 5-9 h, and cooling to room temperature; 3) filtering and dialyzing the solution obtained in the step 2), and obtaining a pure 5-FICD solution; and 4) freeze-drying the solution obtained in the step 3), and obtaining the product. The method takes anticancer drug 5-fluorouracil and photosensitizer indocyanine green as precursors, synthesizes a low-toxicity red light carbon dot through a simple hydrothermal method, improves the shortcoming that a chemotherapy drug has a large side effect, and realizes the targeted killing of hepatocellular carcinoma cells.

The present invention provides a method for manufacturing a drug-coated balloon and a drug-coated balloon obtained by the method. The method for manufacturing a drug-coated balloon is used to apply a drug coating on the surface of a balloon body prepared in advance and in a filled and expanded state, and the anti-proliferative drug component in the drug coating is one or more of nimustine, carmustine, 5-fluorouracil, fluguanosine, gemcitabine, daunorubicin, doxorubicin, paclitaxel, vinblastine, topotecan, aminoglutethimide, sirolimus, everolimus, and zotarolimus. The drug-coated balloon prepared by the method can effectively ensure that when the balloon enters the human body, the thickness of the drug coating on the balloon surface is more uniform and consistent, thereby improving the clinical use effect.

The application belongs to the technical field of medicine, and relates to a use of minocycline in preparation of an antitumor synergist. The minocycline, as the antitumor synergist, has a synergistic effect with 5-fluorouracil and gemcitabine, significantly enhances the curative effect of an antitumor drug, reduces the dosage of the antitumor drug, and reduces side effects of the antitumor drug on the body or damage of the antitumor drug to normal tissue cells.

The application belongs to the technical field of medicine preparation, and particularly relates to a magnetic layered double hydroxide, a targeted drug-loaded nano preparation, a preparation method and application of a tumor-targeted drug-loaded nano preparation. The preparation method of the magnetic layered double hydroxide provided by the application can prepare Fe3O4 nanoparticles with small particle size, and further prepare the magnetic layered double hydroxide which can be used as a water-soluble drug carrier. The magnetic layered double hydroxide is used for preparing the targeted drug-loaded nano preparation and the tumor-targeted drug-loaded nano preparation, and can be used for delivering water-soluble drugs such as 5-fluorouracil. The tumor-targeted drug-loaded nano preparation has good dispersity and can be actively targeted to HepG2 cells with high FR expression, has a good inhibitory effect on liver cancer cells, and is expected to provide a potential new treatment system for magnetic chemotherapy.

An implant device for an eye disease to be inserted into an eyeball may include: a tube having one end to be inserted into an anterior chamber of the eyeball, the tube including a hollow portion through which aqueous humor is drained; and a matrix coupled to an outer surface of the tube and formed of a material capable of impregnating and releasing a drug. At least a part of the matrix may have a cross-section larger than a diameter of the tube. When the implant device for an eye disease is used, an antifibrotic agent, such as dexamethasone, mitomycin-C (MMC), 5-fluorouracil (5-FU), triamcinolone (TA), an anti-vascular endothelial growth factor (VEGF) inhibitor, or a transforming growth factor-beta-beta (TGF-β) inhibitor may be loaded on the matrix, and the antifibrotic agent may be released to surrounding tissue from the matrix after the implant device is inserted.

The present invention belongs to the technical field of pharmaceutical chemistry, and discloses a paeonol Mannich base-rhein conjugate, a preparation method thereof and an application thereof. The conjugate is a compound represented by the general formula (I) or (II) or a pharmaceutically acceptable salt thereof. Compared with the clinically commonly used anti-tumor drugs fluorouracil and paeonol, the conjugate of the present invention has significantly higher in vitro proliferation inhibitory activities against human liver cancer cells (HepG2) and human lung cancer cells (A549), and the in vitro proliferation inhibitory activities of most compounds against human cervical cancer cells (Hela), human colon cancer cells (HT29) and human osteosarcoma cells (U2OS) are significantly better than those of fluorouracil and paeonol, indicating excellent anti-tumor effects. Moreover, the conjugate of the present invention has good water solubility and is expected to be applied to the treatment of various cancers such as cervical cancer, colon cancer, osteosarcoma, lung cancer or liver cancer, and has broad clinical application prospects.

This invention provides a sample pretreatment method and identification method for identifying ginseng polysaccharides in compound fluorouracil oral solution, belonging to the field of pharmaceutical detection and analysis technology. The sample pretreatment method of this invention includes: centrifuging the compound fluorouracil oral solution and taking the clear solution; adding silica gel to the clear solution, mixing, and removing the solvent to obtain a solid mixture; adding ethanol solution or anhydrous ethanol to the obtained solid mixture, heating and refluxing, discarding the ethanol solution, and obtaining the residue; adding water to the obtained residue, sequentially extracting and centrifuging, taking the supernatant obtained by centrifugation, removing the solvent from the supernatant, and then redissolving it with water; the identification method of this invention is thin-layer chromatography analysis, and the developing solvent includes the following components in parts by volume: 6.8-9.2 parts of n-propanol, 1.76-2.24 parts of water, 0.75-1.24 parts of ethyl acetate, and 0.75-1.24 parts of glacial acetic acid. The sample pretreatment method and identification method for identifying ginseng polysaccharides in compound fluorouracil oral solution of this invention have high specificity.

The invention relates to the technical field of pharmaceutical engineering, in particular to a fluorouracil production process which specifically comprises the following condensation reaction steps: S1, adding a base catalyst into dichloromethane, and dropwise adding ethyl formate and ethyl fluoroacetate to obtain a mixture, the mass of the dichloromethane is 3-7 times that of the ethyl fluoroacetate, and the molar equivalence ratio of the added base catalyst to the ethyl formate to the ethyl fluoroacetate is (2.5-3.5): 2.5: 1; s2, controlling the temperature of the mixture obtained in S1 to 30-40 DEG C, and continuously stirring to react for 0.5-2 hours to obtain an intermediate state substance; according to the production process of the fluorouracil, provided by the invention, the production cost during mass production can be remarkably reduced, and meanwhile, the quality and the stability of the fluorouracil product are ensured.

The application belongs to the technical field of biological medical materials, and provides a preparation method of an E. coli drug preparation with photosensitive drug release, which comprises the following steps: incubating photosensitizer Ce6 nanoparticles and E. coli carrying 5-fluorouracil and extract of Prunella vulgaris to obtain the drug preparation; wherein the E. coli carrying 5-fluorouracil and extract of Prunella vulgaris is obtained by using a high-voltage electroporation method to transfer 5-fluorouracil and extract of Prunella vulgaris into the E. coli; the photosensitizer Ce6 nanoparticles are prepared by adding tripolyphosphate to a Ce6 chitosan solution; and the extract of Prunella vulgaris is obtained by extracting Prunella vulgaris with water, concentrating and drying the extract. The traditional antitumor drug 5-fluorouracil and the extract of Prunella vulgaris are matched with each other, and a synergistic effect in the aspect of antitumor is generated, thereby providing a certain reference value for development of a new antitumor drug combination and preparation.

The present invention belongs to the field of medicine and specifically relates to the use of a combination of astemizole and terfenadine in the preparation of a drug for treating gastric cancer. The present invention finds that the antihistamine drug terfenadine can enhance the inhibitory effect of astemizole on gastric cancer AGS and HGC27 cells, significantly inhibiting the proliferation of AGS and HGC27 gastric cancer cells. Furthermore, terfenadine and astemizole can inhibit the migration of gastric cancer cells, induce apoptosis of gastric cancer cells, and block the cell cycle. The effect of terfenadine and astemizole in inhibiting the proliferation of gastric cancer cells is superior to that of the commonly used clinical anticancer drug 5-fluorouracil (5-FU), and the present invention has good application prospects in the treatment of gastric cancer.

The invention discloses a NO / 5-fluorouracil double-delivery system based on Zn-MOF and application of the NO / 5-fluorouracil double-delivery system. A preparation method of the NO / 5-fluorouracil double-delivery system comprises the steps that IRMOF-3 serves as a carrier, 5-fluorouracil is loaded through physical adsorption, NO is loaded in a covalent binding mode under high pressure, and the pH-responsive double-drug delivery system IRMOF-3-NONO-5-FU is constructed. Experiments show that IRMOF-3-NONO (at) 5-FU has pH response release ability, efficient release of 5-FU and NO can be realized in a simulated tumor microenvironment (pH 5), and release of the IRMOF-3-NONO (at) 5-FU is significantly inhibited in a normal physiological environment (pH 7.4); a tumor cell toxicity test shows that the 5-fluorouracil and NO in the IRMOF-3-NONO-5-FU have a synergistic anti-tumor curative effect, and potential clinical application prospects are achieved.

The invention belongs to the field of medicines, and discloses a composition for treating and / or preventing tumors and application thereof. The composition comprises any one of the following pharmaceutical compositions: (1) an ID1 inhibitor and a chemotherapeutic drug; and (2) an ID1 inhibitor and an immune checkpoint inhibitor drug. The chemotherapeutic drug is prepared from 5-fluorouracil, oxaliplatin, capecitabine or irinotecan. The immune checkpoint inhibitor drug is selected from a targeted CTLA-4 antagonistic antibody. The composition disclosed by the invention is an anti-tumor pharmaceutical composition for inhibiting ID1 activity, and experimental verification finds that the composition can improve the chemotherapy treatment effect or immunotherapy effect of tumor patients, so that a theoretical basis is laid for formulating a clinical anti-tumor treatment strategy, and the composition has a wide application prospect.

A pharmaceutical composition for tumor vascular occlusion according to an exemplary embodiment may include alkaline 5-fluorouracil and glucose. For example, the composition may include glucose which exerts a synergistic effect on inducing apoptosis of vascular endothelial cells with alkaline 5-fluorouracil, thereby significantly enhancing the anti-cancer effect.

The invention specifically discloses a PreTA inhibitor and application thereof, and relates to the technical field of biological medicines. The inhibitor provided by the invention can be used for effectively inhibiting the activity of PreTA, so that the anti-tumor effect of 5-fluorouracil (5-FU) is recovered.

The application discloses a method for catalytically producing 5-fluorouracil and application, and belongs to the technical field of biology. The method uses 5-fluoroorotic acid as a substrate and orotidine-5'-phosphate decarboxylase as a catalyst to efficiently catalyze the synthesis of 5-fluorouracil. The catalytic efficiency is further improved by molecular modification of orotidine-5'-phosphate decarboxylase, the efficient and green production of 5-fluorouracil is realized, and the application of 5-fluorouracil in the fields of medicine and the like is promoted.

The application relates to a pharmaceutical cocrystal of cytarabine and 5-fluorouracil and a preparation method thereof, and relates to the technical field of pharmaceutical cocrystals. The pharmaceutical cocrystal is composed of one cytarabine molecule and one 5-fluorouracil molecule as a basic structural unit, and has a chemical formula of [C9H 13 N3O5.C4H3N2O2F]; the pharmaceutical cocrystal belongs to an orthorhombic system and has a space group of P212121. The pharmaceutical cocrystal prepared by a solvent evaporation method and a cooling method improves the permeability of cytarabine, appropriately reduces the solubility of cytarabine, and significantly improves the antitumor activity of cytarabine; through the complementary advantages of the properties and the pharmacodynamic effects of two components, the synergistic antitumor effects of cytarabine and 5-fluorouracil are realized, and a new idea is provided for developing synergistic antitumor pharmaceutical cocrystals. The pharmaceutical cocrystal can keep the skeleton structure of the crystal unchanged after long-term placement at room temperature, the preparation method is simple and easy to implement, the cost is low, and the pharmaceutical cocrystal is convenient for large-scale production.

The invention discloses synthesis and antitumor activity research of a novel drug small molecular formula (1) containing an indole structure, wherein R is as follows: 5-acetylvaleric acid is used as a starting raw material, then Fischer reaction, methylation reaction and hydrolysis reaction are performed to obtain 4-(5-(tert-butyl)-1, 2-dimethyl-1H-indole-3-yl) butyric acid, and the 4-(5-(tert-butyl)-1, 2-dimethyl-1H-indole-3-yl) butyric acid is used as a raw material. The compound is coupled with different amine compounds to obtain a target compound. A target compound is subjected to a CCK-8 experiment, and a conclusion is obtained that the target compound 6f and 5-fluorouracil are tested at the concentration of 20 [mu] M within 6a-6 h, and it can be known that the compound 6f has the best inhibition effect on A549 cells, Hela cells and A549 cells. IC50 value calculation is carried out on a target compound under various concentrations, the IC50 value of 6c to Hep G2 cells is minimum and the inhibition effect is best, and the IC50 value of 6f to A549 cells and Hela cells is minimum and the inhibition effect is best.

Disclosed are method of treating a subject in need thereof comprising applying an alternating electric field, at a frequency for a period of time, to a target site of the subject in need thereof; and administering a combination of leucovorin calcium, fluorouracil, irinotecane hydrochloride, and oxaliplatin to the subject in need thereof. Disclosed are methods of reducing viability of cancer cells comprising applying an alternating electric field, at a frequency for a period of time, to a population of cancer cells; and contacting the population of cells with a combination of leucovorin calcium, fluorouracil, irinotecane hydrochloride, and oxaliplatin. Disclosed are methods of increasing apoptosis of cancer cells comprising applying an alternating electric field, at a frequency for a period of time, to a population of cancer cells; and contacting the population of cancer cells with a combination of leucovorin calcium, fluorouracil, irinotecane hydrochloride, and oxaliplatin. Disclosed are methods of reducing the number of cancer cells comprising applying an alternating electric field, at a frequency for a period of time, to a population of cancer cells; and contacting the population of cancer cells with a combination of leucovorin calcium, fluorouracil, irinotecane hydrochloride, and oxaliplatin.

This invention discloses a method for scalable preparation of 5-fluorouracil-loaded lyophilized nanoparticles. The method first involves self-assembling 5-fluorouracil into a polymer carrier to form core-shell nanoparticles. Then, the hydrophobic core-shell nanoparticles undergo a double emulsification-isothermal evaporation process to form hydrophilic micro / nanoparticles. Finally, D-mannose is assembled onto the surface of the micro / nanoparticles, followed by gradient freeze-drying to prepare PLGA / 5-FU-loaded lyophilized nanoparticles. This method offers advantages such as simple operation, scalability, and good reproducibility. The 5-FU drug in the prepared lyophilized nanoparticles exhibits good crystallinity. During the inhibition of pancreatic cancer cell growth, it effectively improves the bioavailability, biocompatibility, and physical stability of 5-fluorouracil, significantly inhibiting pancreatic cancer cell growth and demonstrating high anti-tumor immunomodulatory properties.

The invention discloses a preparation method of a 5-fluorouracil / high impact polystyrene anti-tumor implantation stent. The preparation method comprises the following steps: S1, uniformly mixing 5-fluorouracil with the mass fraction of 0.5%-1% and high impact polystyrene granules with the mass fraction of 99%-99.5%; s2, a screw extruder and a traction machine are cooperatively used, and the raw materials obtained in the step S1 are prepared into a uniform and smooth wire rod with the specific diameter through the hot melt extrusion technology; and S3, printing an anti-tumor stent entity by using the wire obtained in the step S2 through a 3D printing technology. The prepared 5-fluorouracil / high impact polystyrene anti-tumor implant stent has certain biocompatibility, high drug bioavailability and certain slow release effect, can effectively induce death of cancer cells and inhibit growth of tumors, and meanwhile, reduces toxic and side effects of anti-cancer drugs.

The invention relates to an oligonucleotide lung targeting delivery system and application thereof in treatment of lung diseases, and relates to the technical field of biological medicines and nano-medicines. The invention designs a high-efficiency lung targeting oligonucleotide delivery drug, which comprises lipid nanoparticles, the lipid nanoparticles contain oligonucleotide and lipid components, and the lipid components are composed of 4-(N, N-dimethylamino) butyric acid (dilinoleyl) methyl ester, (2, 4-dimethylamino) butyric acid (dilinoleyl) methyl ester, (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid The composition is composed of 1, 3-dioleoyl-propyl)-trimethylamine, dipalmitoyl phosphatidylcholine and pegylated lipid. A breakthrough of a nucleic acid medicine lung delivery technology is realized, in-vivo experiment verification results show that the lung aggregation efficiency is improved by about 2-4 times compared with that of traditional lipid nanoparticles, the lipid nanoparticles have remarkable lung metastatic tumor resisting activity, in-vivo experiments show that the lipid nanoparticles can inhibit growth of colorectal cancer lung metastatic tumors and prolong the survival time of mice, and the lipid nanoparticles have good application prospects. And the effect is better than that of 5-fluorouracil and regorafenib.

The invention belongs to the technical field of biological medicine, and particularly discloses fluorouracil sustained-release nano-microspheres as well as a preparation method and application thereof. The preparation method comprises the following steps: S1, dissolving fluorouracil in a polyarginine aqueous solution, uniformly stirring, and adjusting the pH value to 7.2-7.4 to obtain a fluorouracil solution; s2, dissolving amphiphilic alginate in water, sequentially adding carboxymethyl chitosan and quaternized gelatin, and uniformly stirring to obtain a composite carrier solution; and S3, mixing the fluorouracil solution obtained in the step S1 with the composite carrier solution obtained in the step S2, performing ultrasonic treatment, performing self-assembly, performing centrifugation, and collecting precipitates to obtain the fluorouracil nano-microspheres. The invention discloses a fluorouracil sustained-release nano-microsphere as well as a preparation method and application thereof. The fluorouracil sustained-release nano-microsphere can be used for remarkably improving the encapsulation efficiency and the drug loading capacity of fluorouracil, realizing long-acting sustained release of drugs, enhancing the tumor targeting property and the cell uptake efficiency and improving the treatment effect.

The present invention belongs to the field of biomedical technology, and particularly relates to a pyridinecarboxylic acid alkaloid, its preparation method and application. This compound can be obtained by using a fungus derived from sea lilies in the South China Sea through modern microbial fermentation engineering technology, and it is easy to achieve large-scale industrial production. Moreover, it is found through research that the pyridinecarboxylic acid alkaloid compound has a significant inhibitory effect on gastric cancer cells, can significantly inhibit the activity and clone formation of gastric cancer cells, promote the apoptosis of gastric cancer cells, and reduce the invasion of gastric cancer cells; when the pyridinecarboxylic acid alkaloid compound and a first-line clinical chemotherapy drug such as 5-fluorouracil act on gastric cancer cells in combination, the cell inhibition effect is also significantly improved, showing a synergistic anti-gastric cancer effect.

The present invention discloses the use of a lncRNA IGFL2-AS1 gene inhibitor in the preparation of a drug for treating lung cancer. The nucleotide sequence of the lncRNA IGFL2-AS1 gene is shown in SEQ ID NO.1. The lncRNA IGFL2-AS1 gene inhibitor is a small interfering RNA that uses the IGFL2-AS1 gene or its transcript as an inhibition target or a silencing target. The nucleotide sequence of the shRNA of the small interfering RNA is shown in SEQ ID NO.17 or SEQ ID NO.18. IGFL2-AS1 is mainly localized in the cell nucleus and expressed in a small amount in the cytoplasm. IGFL2-AS1 can promote the proliferation, migration and drug resistance of non-small cell lung cancer A549 and H520 cells. Targeted inhibition of IGFL2-AS1 can significantly reduce the drug resistance of lung cancer cells to cisplatin or 5-fluorouracil.